PHARMACOLOGICAL STUDIES ON TRIAZINE DERIVATIVES V. SEDATIVE AND NEUROLEPTIC ACTIONS OF 2-AMINO-4-[4-(2-HYDROXYETHYL)-PIPERAZIN-1-YL]-6-TRIFLUOROMETHYL-s-TRIAZINE (TR-10)

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Pharmacological properties of 2-amino-4-[4-(2-hydroxyethyl)-piperazin-1-yl]-6-trifluoromethyl-s-triazine (TR-10) were investigated in mice and rats. Chlorpromazine served as a reference compound. TR-10 expressed in general the pharmacological profiles as neuroleptics ascertained by anti-methamphetamine activity, supression of conditioned avoidance response, taming effects, decrease in exploratory behavior and cataleptogenic activity. Among these effects, anti-methamphetamine action was most potent. Different from chlorpromazine, TR-10 showed a similar pharmacological activity pattern in the intraperitoneal and oral routes of adminisstration as depicted from ED50/LD50 values. Although the effects relevant to neuroleptics were less potent than chlorpromazine, such were seen with TR-10 at lower doses than those causing muscle relaxation. TR-10 significantly depressed the spontaneous motor activity but showed no anti-convulsant action in mice. Hypothermic action, potentiating effects of hypnotics and α-adrenergic blocking action, characteristic to chlorpromazine, were very weak for TR-10. TR-10 also showed low toxicity in mice (LD50=820 mg/kg p.o., 465 mg/kg i.p.) compared with that of chlorpromazine (LD50 =370 mg, kg p.o., 228 mg/kg i.p.).
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